Plaque-disclosing composition and package system

ABSTRACT

A plaque-disclosing formulation suitable for use in aerosol form without causing undue &#39;&#39;&#39;&#39;cold-sensitivity&#39;&#39;&#39;&#39; -related pain to a patient. The formulation comprises a specially selected dye such as Erythrosine B, and an active solvent like ethanol to aid penetration of the dye into the plaque deposit. It is incorporated into an aerosol charge which comprises a Freon-type propellant in a quantity which contributes less than 50 B.t.u. heat of evaporation per pound of total aerosol charge at one atmosphere. It is advantageously packaged in an aerosol-type container equipped with a meter-type valve rated for discharging less than about 70 milligrams per shot. The container should be equipped with a discharge conduit of from 1.5 to 2.5 inches in length and a bore size of from about 0.010 to about 0.03 inches in diameter.

United States Patent Max J. Perlitsh 20 Everett Ave., Winchester, Mass.01890 [211 App]. No. 53,519

[22] Filed July 6, 1970 [45] Patented Nov. 30, 1971 [72] lnventor [56]References Cited UNITED STATES PATENTS 1,112,180 9/1914 WestenfelterPrimary Examiner-Shep K. Rose Attorney-Cesari and McKenna ABSTRACT: Aplaque-disclosing formulation suitable for use in aerosol form withoutcausing undue "cold-sensitivity -related pain to a patient. Theformulation comprises a specially selected dye such as Erythrosine B,and an active solvent like ethanol to aid penetration of the dye intothe plaque deposit. It is incorporated into an aerosol charge whichcomprises a Freon-type propellant in a quantity which contributes lessthan 50 B.t.u. heat of evaporation per pound of total aerosol charge atone atmosphere. It is advantageously packaged in an aerosol-typecontainer equipped with a meter-type valve rated for discharging lessthan about 70 milligrams per shot. The container should be equipped witha discharge conduit of from 1.5 to 2.5 inches in length'and a bore sizeof from about 0.010 to about 0.03 inches in diameter.

PATENIEU NUV30 IQYI FIG. 1

MAX J. PERLITSCH lnven/or CESAR! 8 MCKENNA A horneys PLAQUE-DISCLOSINGCOMPOSITION AND PACKAGE SYSTEM BACKGROUND OF THE INVENTION A number ofdiseases of the teeth and/or gums are related to 5 the presence ofcertain types of bacteria found in the mouth. Tooth decay as manifestedby cavities and pyorrhea are common examples of bacteria-caused dentaldiseases.

The harmful bacteria tend to attach themselves to the teeth 10 themouth. This acid production will normally continue in and l5 on thebacterial deposit for a considerable time after the sugar has beeneaten, causing tooth decay.

Plaque, if not removed from the mouth, will eventually form a relativelyhard, tenaciously adherent deposit called calculus or tartar. Thiscalculus deposit itself becomes a favorable en- 2 vironment for thecolonization of more bacteria and, consequently, the size of thecalculus deposit tends to increase as further layers of plaque form andcalcify thereon. Eventually this calculus and plaque cause irritationwhich leads to infection of the gum tissue. Although the earliestmanifestation of such irritation and infection may be bleeding of gumtissue, the infection will eventually reach the bone that supports theteeth and contribute to a progressive loss of the bone support of theteeth and, consequently, to the loss of the teeth.

For these reasons, plaque-control is becoming recognized as a basicrequirement of preventive dentistry. It has become recognized that, byfrequently removing dental plaque from his teeth, a person will be ableto effectively avoid the two most common dental diseases such as toothdecay and pyorrhea.

The growth of plaque and the subsequent buildup of calculus deposits,can be avoided by proper oral hygiene practices which may be carried outby a person on his own teeth. Of course such self-care pre-assumes thata person start with relatively clean teeth, i.e., teeth from whichplaque and calculus deposits have been recently cleaned. Such self-carealso preassumes the ability by the person to identify those portions ofhis mouth where the plaque is beginning to build up once again. ln thisconnection, it is to be emphasized that plaque is sufficiently adhesivethat normal nonlocalized care is ineffective and burdensome to a personwishing to remove plaque from selected locations in his mouth.Unfortunately plaque is difficult to see even on the exposed surfaces ofthe teeth because it is usually deposited in a colorless and transparentform. Therefore it has been generally regarded to be desirable to useplaque disclosing" compositions to identify areas of the mouth whereplaque buildup is a problem.

Among suggested plaque disclosing compositions have been solutions ofbasic fuschsin dye which have been painted on the tooth surface withcotton applicators. These solutions have the general drawback of beingnondiscriminating discriminating in that they tend to stain other partsof the mouth as well as plaque deposits for up to several hours afteruse. This presents a real problem in terms of acceptance because of thecosmetic problems presented to the user.

Another attempted solution to the problem has been the incorporation ofvarious dyes in chewable wafers. Frequently such wafers do not developsufficient concentration of dye to stain the plaque deposits. Moreover,the activity of the dye compositions generated in the mouth is so lowthat the dye does not adequately penetrate the plaque deposit and theyare not detected by the user of the wafer. Thus a person can easily bemisled into believing he has cleaned the plaque from his teeth whensuch, in fact, is not the case. It remains a problem, then, to providepeople with plaque-disclosing means that can be conveniently andeffectively used by people without a detrimental cosmetic effect.

SUMMARY OF THE INVENTION It is an object of the invention to provide animproved plaque-disclosing means which selectively identifies areas ofplaqueformation on all tooth surfaces.

It is another object of the invention to provide an improvedplaque-disclosing composition which combines the ability to penetrateplaque deposits and yet is susceptible to relatively easy removal fromthe mouth by washing and rinsing after use.

Another object of the invention is to provide a novel process for safelyand easily applying plaque-disclosing compositions in such a way as toassure the discrimination between plaque-contaminated and plaque freesurfaces.

A further object of the invention is to provide a suitable dispenser foruse in the aforesaid process.

Still another object of the invention is to achieve a means for applyinga plaque-disclosing composition in a spray form while substantiallyachieving the above objects, but without causing pain to the patientbecause of cold-sensitivity of the 0 teeth.

Other objects of the invention will be obvious to those skilled in theart on reading the instant invention.

The above objects have been substantially achieved by the formulation ofan improved plaque-disclosing formulation and the incorporation of thisformulation in a novel composition suitable for application as anaerosol spray. The aerosol composition comprises a carefully selectedpropellant which gives adequate spray coverage with a minimum ofinterference with the plaque-disclosing formulation yet evaporates insuch a way as to minimize the discomfort of patients havingcold-sensitivity problems.

The plaque-disclosing formulation includes a dye, and a solvent which isadapted to dissolve the dye and to aid the penetration of the dye intothe plaque deposit.

The most advantageous dye for use in the plaque-disclosing formulationis selected from those dyes such as Erythrosine B. This dye is an acidred dye of the Xanthene type which is further identified as F.D. & C.Red No. 3 and Dye No. 45430 in the Color Index.

Erythrosine B exhibits a significantly superior performance over suchdyes as basic fuchsin which stains so intensively that an excessivelyprolonged staining effect is realized. Moreover, such dyes as amaranthand Brilliant Blue are excessively water soluble and neither penetratenor persist in the mouth to the degree desirable for plaque-disclosingpurposes.

It has been found that from about 0.5 percent to 10 percent by weight ofdyestuff should be used in the plaque-disclosing composition, mostadvantageously about 1.5 to 3 percent. The balance of theplaque-disclosing composition is the solvent for the dye.

The solvent must, of course, be selected from those that arephysiologically tolerable with reference to the particular oral utilityof the invention. The solvent must also provide a major portion of amore active component to facilitate the solution of a dye (which musthave some resistance to water leaching) and to aid the penetration ofthe dye into plaque deposits. The use of a physiologically intolerablealiphatic hydroxy compound such as ethanol is particularly advantageous.ln addition to this more active component, the solvent should comprise asubstantial quantity of water to facilitate removal of the dyestuff fromthe areas of the mouth where the more active solvent component does notfind plaque deposits into which it carries the dyestuff. Otherwater-soluble, physiologically tolerable solvents such as glycerine canbe used although the ethanol-water system gives the best balance betweenplaque discrimination and dye penetration under most conditions of use.

In summary the plaque-disclosing formulation comprises a dyestuff, asolvent comprising a more active component (or penetrant) such as ethylalcohol and a less active component such as water. The plaque-disclosingformulation most advantageously used with Erythrosine B is a mixture ofaliphatic alcohol, preferably ethanol, and water.

The total aerosol composition comprises a carefully selected propellantto act as a carrier of the plaque-disclosing formulation. Thispropellant must be carefully selected to avoid causing pain to thosepatients having what is known to dentists as cold-sensitivity." To thisend, it is advantageous that the propellant have a maximum heat ofevaporation of about 50 B.t.u. per pound of total aerosol composition atl atmosphere of pressure. It is advantageous for this value-which is ameasure of the cooling capacity of the solvent-to be much closer to 20B.t.u. per pound of aerosol composition charge.

The propellant system, of course must be one which lacks toxiccharacteristics. A particularly advantageous propellant systemconforming to the criteria set forth above and selected from thehalogen-substituted hydrocarbon-type compounds available from E.1.DuPont de Nemours Company under the trade designation Freon. Among suchsystems would be a 60:40 mixture of CCllflCClF and CCI F or plain CCl Feach, of course, taken in an appropriate quantity.

The total propellant forms about 30 to 60 percent of the entire aerosolspray composition with the more advantageous range being from about 30to 50 percent. The lower quantity reduces the amount of gas which mustbe dissipated from the sometimes restricted volume adjacent thedischarge point.

The means by which the above-disclosed aerosol formulation is deliveredto the desired surfaces inside the mouth has been found to be important,not only to allow manipulative convenience in applying theplaque-disclosing solution to a particular tooth surface within themouth, but also to provide a means to further reduce thecold-sensitivity problem by preconditioning and moderating the preciserate at which the aerosol solution is discharged from the device. lnthis regard, it has been discovered that single discharges of aerosolcomposition should be made in quantities of from about 20 to about 70milligrams with the lower discharges being preferred.

Moreover, the length of the applicator arm and bore therein have beenfound to provide the most advantageous spray when so designated as to befrom about 1.5 inches to 2.5 inches in length and having a bore size offrom about 0.010 inch to about 0.03 inch. These bore sizes and lengthprovide a balance between velocity and shape of the spray as it leavesthe bore discharge and aid in obtaining not only the desired directionaleffect but a suitable evaporation of propellant before the spray hitsthe tooth surface.

ILLUSTRATIVE EXAMPLE OF THE INVENTION EXAMPLE 1 The following aerosolcomposition was prepared:

1 by welght Erythrosine B Dye 1 Delomzed water 1 S Ethanol solvent 37 5Freon l2 (CCIJQ) 20,0 Freon 114(CC1F,CC1F,1 30.0

The solvent (SDA 38 8) used was a preflavored solvent conforming to theStandurds for Denatured Alcohol 38 B per the Food the DrugAdministration standards This aerosol composition was charged into anaerosol package 10, as shown in P16. 1, comprising an Emson ASD-l valveactuator 11 and a valve system which metered 50 milligrams of material13 through a 2.25-inch arm 12 having a 0.018-inch bore 14 therein. Arm12 is fitted with a protective cap 16. The resulting package assemblyprovides a sealed nonbreakable package which can easily be used to applythe plaque-disclosing composition in a high concentration to a localizedand preselected area. Moreover, the container is substantially air free,thereby assuring minimum oxidative degradation of the dyestuff. Thevelocity imparted by the propellant to the alcohol-dye allowed theinstantaneous disclosure of the plaque deposits without risk of"false-negatives" of the type frequently encountered when so-calleddisclosing-wafers are used.

EXAMPLE 2 The following aerosol charge was prepared:

This material had the advantages of the composition disclosed in example1 except that it was improved with respect to limiting undesirableresponses to cold sensitivity because of the lower concentration ofpropellant. The latent heat of evaporation was only about 24 B.t.u. perlb. of aerosol charge. Therefore the propellant flashed off as it camefrom the nozzle with minimum of local cooling effect.

It is to be understood that the following claims are intended to coverall of the generic and specific features of the invention hereindescribed.

What is claimed is:

l. A plaque-disclosing aerosol dispenser package equipped with ametering valve and a discharge arm having a bore size and length formingmeans to provide a suitable evaporation and dissipation of propellentgas before aerosol spray discharged therefrom hits a tooth surface, saidpackage con taining a composition comprising (A) Erythrosin B as theessential plaque-disclosing dye, (B) a physiologically tolerable solventtherefore consisting of:

l a major quantity of plaque-penetrating alcohol and 2. a minor quantityof water in admixture with (C) an effective quantity of nontoxichalogenated hydrocarbon propellant, said propellant contributing notabove 50 B.T.U.s of heat of evaporation to each pound of the totalaerosol formulation, said composition being substantially free ofexcessively prolonged and insufficiently persistent plaque-disclosingdyes and being free of propellants contributing sufficient heat ofevaporation to cause painful sensation on teeth.

2. A plaque-disclosing composition as defined in claim 1 wherein saiddye forms from 0.5 to 10 percent of said composition and said alcohol isethanol.

3. A plaque-disclosing composition as defined in claim 2 wherein theweight ratio of ethanolzwater is at least 2:1 and the dye forms from 1.5to 3 percent of said composition.

4. A process for the selective disclosure of plaque deposits by aerosoltechniques without subjecting a patient to pain caused by localizedcooling, said process comprising the steps of spraying a discharge of aneffective amount of a dye-bearing solution as defined in claim 1 fromthe discharge arm of the aerosol dispenser package of claim 1.

5. A process as defined in claim 4 wherein said dye is Erythrosyne B,and wherein said active solvent component is ethanol.

6. A dispenser package as defined in claim 1 useful in the selectivedisclosure of plaque deposits by aerosol techniques and comprising theplaque-disclosing aerosol formulation in an aerosol dispenser equippedwith a metering valve capable of ejecting from about 20 to about 70milligrams of said formulation per discharge and equipped with adischarge arm of from 1.5 to 2.5 inches in length having therein aconduit bore 5 of from 0.01 inch to about 0.03 inches in diameter.

2. a minor quantity of water in admixture with (C) an effective quantityof nontoxic halogenated hydrocarbon propellant, said propellantcontributing not above 50 B.t.u.s of heat of evaporation to each poundof the total aeRosol formulation, said composition being substantiallyfree of excessively prolonged and insufficiently persistentplaque-disclosing dyes and being free of propellants contributingsufficient heat of evaporation to cause painful sensation on teeth.
 2. Aplaque-disclosing composition as defined in claim 1 wherein said dyeforms from 0.5 to 10 percent of said composition and said alcohol isethanol.
 3. A plaque-disclosing composition as defined in claim 2wherein the weight ratio of ethanol:water is at least 2:1 and the dyeforms from 1.5 to 3 percent of said composition.
 4. A process for theselective disclosure of plaque deposits by aerosol techniques withoutsubjecting a patient to pain caused by localized cooling, said processcomprising the steps of spraying a discharge of an effective amount of adye-bearing solution as defined in claim 1 from the discharge arm of theaerosol dispenser package of claim
 1. 5. A process as defined in claim 4wherein said dye is Erythrosyne B, and wherein said active solventcomponent is ethanol.
 6. A dispenser package as defined in claim 1useful in the selective disclosure of plaque deposits by aerosoltechniques and comprising the plaque-disclosing aerosol formulation inan aerosol dispenser equipped with a metering valve capable of ejectingfrom about 20 to about 70 milligrams of said formulation per dischargeand equipped with a discharge arm of from 1.5 to 2.5 inches in lengthhaving therein a conduit bore of from 0.01 inch to about 0.03 inches indiameter.